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Bioavailable Curcumin for Pain

Curcumin Curcumin
Longevity By Nature
 
EuroMedica

Turmeric, and more specifically its primary active constituent known as curcumin, has been used extensively in ancient and modern times for its medicinal qualities.1,2 Not surprisingly, curcumin is one of the most popular nutraceuticals in use today. In fact, a study3 by Grand View Research, Inc. indicates that the global curcumin market will reach $94.3 million by 2022. This is consistent with Global Market Insights,4 whose data predicts that the global curcumin market will exceed $100 million by 2024. Research has demonstrated a wide spectrum of biological actions for curcumin, including anti-inflammatory, antioxidant, anticarcinogenic, antimutagenic, anticoagulant, antifertility, antidiabetic, antibacterial, antifungal, antiprotozoal, antiviral, antifibrotic, antivenom, antiulcer, hypotensive and cholesterol lowering activities.5 The focus of this article is on curcumin’s benefits for pain—with a focus on sports performance.

Curcumin Bioavailability

Before proceeding to a discussion of human research on curcumin and pain, let’s first address the fact that curcumin has relatively poor biovailability—with 40 percent to 75 percent of curcumin passing through the digestive tract unchanged in animal research.6 Also, blood concentrations of curcumin are low and tissue distribution is limited following oral dosing due to its fast metabolic turnover in the liver and intestinal wall.7-15 Even upon intake of doses as high as 10 or 12 g curcumin, maximum plasma curcumin concentrations in humans, remain in the low nanomolar range (<160 nmol/L).16

There are, however, a few different commercial curcumin extracts that are supported by research showing better bioavailability vs. regular curcumin. One such extract, whose effects on pain in relation to sports performance will be discussed below, is CurcuWIN, a novel curcumin formulation from OmniActive Health Technologies containing 20 percent curcuminoids. A recent human study17 showed that the absorption of total curcuminoids in the blood of this water-dispersible form of curcumin was 45.9-fold higher than normal curcumin.

High-dose Curcumin Research In on Pain in Sports Performance

To determine effects of curcumin on muscle damage, inflammation and delayed onset muscle soreness (DOMS) in humans, 17 men completed a double-blind randomized-controlled crossover trial18 to estimate the effects of 5 g curcumin supplementation (2.5 g twice daily) versus placebo on single-leg jump performance and DOMS following unaccustomed heavy eccentric exercise. Results were that at 24 and 48-h post-exercise, curcumin facilitated moderate-large reductions in pain during single-leg squat, gluteal stretch and squat jump. A small increase in single-leg jump performance was associated with the pain reduction.

Another randomized, placebo-controlled, single-blind pilot trial19 was conducted with 20 healthy, moderately active male volunteers to test whether 2 g of curcumin phytosome (1 g twice daily) reduce damage from oxidative stress and inflammation related to acute muscle injury induced by eccentric continuous exercise. Supplementation was initiated 48 hours prior to a downhill running test and was continued for 24 hours after the test (four days in total). Results were that subjects in the curcumin group reported less pain in the lower limb as compared with subjects in the placebo group, with significant differences in the right and left anterior thighs. Significantly fewer subjects in the curcumin group had MRI evidence of muscle injury in the posterior or medial compartment of both thighs. Increases in markers of muscle damage and inflammation tended to be lower in the curcumin group.

Low-dose Curcumin Research In on Pain in Sports Performance

In the previous two discussed studies, curcumin was effective in reducing exercise-related pain when used in high doses of 2-5 g daily. But does it have efficacy when used at a lower dose? This was examined in a double-blind, randomized, placebo-controlled study20 with 63 physically active men and women who were randomly assigned to ingest 250 mg of CurcuWIN (50 mg of curcuminoids), 1,000 mg of CurcuWIN (200 mg of curcuminoids), or a corn starch placebo (PLA) for eight weeks. Since it is known that unaccustomed exercise, especially when it has an eccentric component, causes muscle damage and subsequent performance decrements, the current study sought to examine the effect of these two doses of curcumin supplementation on performance decrements following downhill running. Various parameters were examined, including isokinetic peak extension torque.

Isokinetic muscle strength is generally described in units such as peak torque (Nm) and/or peak force (N). The intent of evaluating isokinetic strength is to determine the work capacity of a muscle group or the ability to produce force as well as the balance (ratio) of opposing muscle groups (eg., flexion vs. extension). Muscle dysfunction or weakness then becomes a limitation to functional performance.21

At the end of the supplementation period, subjects completed a downhill running protocol intended to induce muscle damage. Results were that isokinetic peak extension torque did not change in the 200-mg dose, while significant reductions occurred in the PLA and 50-mg groups through the first 24 hours of recovery. Isokinetic peak flexion torque and power both decreased in the 50-mg group, while no change was observed in the PLA or 200-mg groups. These benefits continued 72 hours post exercise.

Improvements in exercise-induced total thigh soreness indicated that the 200-mg groups reported 26 percent, 20 percent, and 8 percent less soreness immediately, 24 hours and 48 hours after exercise, respectively, than the soreness levels that were reported in the PLA and 50-mg groups—although this trend didn’t not reach statistical significance.

Curcumin’s Mechanism of Action

Although the exact mechanism of action for curcumin’s analgesic (pain-relieving) activity is not clear, some evidence from in-vitro research suggests that curcumin can inhibit transient receptor potential vanilloid 1 (TRPV1)-mediated pain hypersensitivity.22 In human research, curcumin inhibits levels of inflammatory markers associated with arthritis, including C-reactive protein, rheumatoid factor and the erythrocyte sedimentation rate.23 Animal models suggest that turmeric extract reduces arthritis-associated joint inflammation by inhibiting NF-kB activation.24 Curcumin also seems to inhibit inflammatory enzymes such as collagenase, elastase and hyaluronidase.25 Additionally, research in humans shows that curcumin reduces the inflammatory markers interleukin-6 and C-reactive protein, but not tumor necrosis factor (TNF)-alpha.26

Conclusion

Curcumin has been used extensively in ancient and modern times for its medicinal qualities and is one of the most popular nutraceuticals in use today. Research has demonstrated a wide spectrum of biological actions for curcumin, including anti-inflammatory and pain-relieving actions. Research has demonstrated that curcumin was effective in reducing exercise-related pain when used in high doses of 2-5 g daily. Although curcumin has poor bioavailability, a novel curcumin formulation (CurcuWIN, from OmniActive Health Technologies) has been shown to have 45.9-fold higher absorption that than normal curcumin. Furthermore, research has demonstrated that 1,000 mg of CurcuWIN daily was effective in improving effects of exercise-related muscle damage and pain.

References

1 Chattopadhyay I, Biswas K, Bandyopadhyay U, Banerjee RK. Turmeric and curcumin: Biological actions and medicinal applications. Current Science. 2004;87(1):44-53.

2 Curcuma longa (turmeric). Monograph. Altern Med Rev 2001;6 Suppl:S62-6.

3 PR Newswire. Curcumin Market is Anticipated to Grow to $94.3 Million By 2022: Grand View Research, Inc. June 22, 2015. Retrieved February 6, 2018 from www.prnewswire.com/news-releases/curcumin-market-is-anticipated-to-grow-to-943-million-by-2022-grand-view-research-inc-508996451.html.

4 Global Market Insights, Inc. Curcumin Market will exceed USD 100 million by 2024. September 21, 2017. Retrieved February 5, 2018 from www.gminsights.com/pressrelease/curcumin-market.

5 Chattopadhyay I, Biswas K, Bandyopadhyay U, Banerjee RK. Turmeric and curcumin: Biological actions and medicinal applications. Curr Sci. 2004;28(1):44-53.

6 Luper S. A review of plants used in the treatment of liver disease: part two. Altern Med Rev. 1999;4:178-188.

7 Shoba G, Joy D, Joseph T, Majeed M, et al. Influence of piperine on the pharmacokinetics of curcumin in animals and human volunteers. Planta Med. 1998;64:353–356.

8 Sharma RA, McLelland HR, Hill KA, Ireson CR, et al., Pharmacodynamic and pharmacokinetic study of oral Curcuma extract in patients with colorectal cancer. Clin. Cancer Res. 2001;7:1894–1900.

9 Vareed SK, Kakarala M, Ruffin MT, Crowell JA, et al. Pharmacokinetics of curcumin conjugate metabolites in healthy human subjects. Cancer Epidemiol. Biomarkers Prev. 2008;17:1411–1417.

10 Cheng AL, Hsu CH, Lin JK, Hsu MM, et al. Phase I clinical trial of curcumin, a chemopreventive agent, in patients with high-risk or pre-malignant lesions. Anticancer Res. 2001;21:2895–2900.

11 Lao CD, Ruffin MT, Normolle D, Heath DD, et al. Dose escalation of a curcuminoid formulation. BMC Complement. Alter. Med. 2006;6:10.

12 Garcea G, Berry DP, Jones DJ, Singh R, et al. Consumption of the putative chemopreventive agent curcumin by cancer patients: assessment of curcumin levels in the colorectum and their pharmacodynamic consequences. Cancer Epidemiol. Biomarkers Prev. 2005;14:120–125.

13 Sharma RA, Euden SA, Platton SL, Cooke DN, et al. Phase I clinical trial of oral curcumin: biomarkers of systemic activity and compliance. Clin Cancer Res. 2004;10:6847–6854.

14 Carroll RE, Benya RV, Turgeon DK, Vareed S, et al. Phase IIa clinical trial of curcumin for the prevention of colorectal neoplasia. Cancer Prev. Res. (Phila) 2011;4:354–364.

15 Ringman JM, Frautschy S A, Teng E, Begum AN, et al. Oral curcumin for Alzheimer’s disease: tolerability and efficacy in a 24-week randomized, double blind, placebo-controlled study. Alzheimers Res. Ther. 2012;4:43.

16 Vareed SK, Kakarala M, Ruffin MT, Crowell JA, et al. Pharmacokinetics of curcumin conjugate metabolites in healthy human subjects. Cancer Epidemiol. Biomarkers Prev. 2008;17:1411–1417.

17 Jäger R, Lowery RP, Calvanese AV, Joy JM, Purpura M, Wilson JM. Comparative absorption of curcumin formulations. Nutr J. 2014 Jan 24;13:11.

18 Nicol LM, Rowlands DS, Fazakerly R, Kellett J. Curcumin supplementation likely attenuates delayed onset muscle soreness (DOMS). Eur J Appl Physiol. 2015 Aug;115(8):1769-77.

19 Drobnic F, Riera J, Appendino G, Togni S, Franceschi F, Valle X, Pons A, Tur J. Reduction of delayed onset muscle soreness by a novel curcumin delivery system (Meriva): a randomised, placebo-controlled trial. J Int Soc Sports Nutr. 2014 Jun 18;11:31.

20 Jäger R, Purpura M, Kerksick CM. Eight Weeks of a High Dose of Curcumin Supplementation May Attenuate Performance Decrements Following Muscle-Damaging Exercise. Nutrients. 2019 Jul 23;11(7). pii: E1692.

21 Horvat M, Pitetti KH, Croce R. Isokinetic torque, average power, and flexion/extension ratios in nondisabled adults and adults with mental retardation. J Orthop Sports Phys Ther. 1997 Jun;25(6):395-9.

22 Yeon, K. Y., Kim, S. A., Kim, Y. H., Lee, M. K., Ahn, D. K., Kim, H. J., Kim, J. S., Jung, S. J., and Oh, S. B. Curcumin produces an antihyperalgesic effect via antagonism of TRPV1. J Dent.Res 2010;89(2):170-174.

23 Amalraj A, Varma K, Jacob J, et al. A novel highly bioavailable curcumin formulation improves symptoms and diagnostic indicators in rheumatoid arthritis patients: A randomized, double-blind, placebo-controlled, two-dose, three-arm, and parallel-group study. J Med Food. 2017;20(10):1022-1030.

24 Funk, J. L., Frye, J. B., Oyarzo, J. N., Kuscuoglu, N., Wilson, J., McCaffrey, G., Stafford, G., Chen, G., Lantz, R. C., Jolad, S. D., Solyom, A. M., Kiela, P. R., and Timmermann, B. N. Efficacy and mechanism of action of turmeric supplements in the treatment of experimental arthritis. Arthritis Rheum. 2006;54(11):3452-3464.

25 Chainani-Wu, N. Safety and Anti-Inflammatory Activity of Curcumin: A Component of Tumeric (Curcuma longa). J Altern. Complement Med. 2003;9(1):161-168.

26 Tabrizi R, Vakili S, Akbari M, et al. The effects of curcumin-containing supplements on biomarkers of inflammation and oxidative stress: A systematic review and meta-analysis of randomized controlled trials. Phytother Res. 2019;33(2):253-262.

Gene Bruno, MS, MHS, the dean of academics for Huntington College of Health Sciences, is a nutritionist, herbalist, writer and educator. For more than 30 years he has educated and trained natural product retailers and health care professionals, has researched and formulated natural products for dozens of dietary supplement companies, and has written articles on nutrition, herbal medicine, nutraceuticals and integrative health issues for trade, consumer magazines and peer-reviewed publications. He can be reached at gbruno@hchs.edu.